The Nitrogen Is Bonded Directly To -c(=x)-, Wherein X Is Chalcogen (e.g., 2 Benzamidomethyl - Pyrrolidines, Etc.) Patents (Class 548/567)
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Patent number: 6348602Abstract: Novel compounds that are potent and selective inhibitors of PIDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.Type: GrantFiled: November 17, 2000Date of Patent: February 19, 2002Assignee: ICOS CorporationInventors: Kerry W. Fowler, Amy Oliver, Joshua Odingo
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Publication number: 20020019536Abstract: The present invention relates to urethanes and the thio and dithio analogues thereof of general formula 1Type: ApplicationFiled: March 24, 1999Publication date: February 14, 2002Inventors: ROLAND MAIER, RUDOLF HURNAUS, MICHAEL MARK, BERNHARD EISELE, PETER MUELLER, GEBHARD ADELGOSS, GEBHARD SCHILCHER
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Publication number: 20020019374Abstract: Salicylohydrazide derivatives of the formula I 1Type: ApplicationFiled: June 14, 2001Publication date: February 14, 2002Inventors: Andreas Gypser, Thomas Grote, Joachim Rheinheimer, Ingo Rose, Peter Schafer, Oliver Cullmann, Markus Gewehr, Wassilios Grammenos, Jordi Tormo i Blasco, Bernd Muller, Hubert Sauter, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Publication number: 20010056185Abstract: Novel C3A ligands are provided. Methods of using the present compounds to treat immune and inflammation disease are also provided.Type: ApplicationFiled: March 12, 2001Publication date: December 27, 2001Inventor: Dennis Lee
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Publication number: 20010056189Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: ApplicationFiled: June 11, 2001Publication date: December 27, 2001Inventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Jeffrey S. Carter, Bryan H. Norma, Balekudru Devadas, Hwang-Fun Lu
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Publication number: 20010051731Abstract: Para-alkyl, aryl, cycloheteroalkyl or heteroaryl [carbonyl or sulfonyl] amino substituted phenyl amides active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.Type: ApplicationFiled: May 1, 2001Publication date: December 13, 2001Inventors: Fred T. Bizzarro, Nancy-Ellen Haynes, Ramakanth Sarabu
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Patent number: 6323223Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: August 14, 1998Date of Patent: November 27, 2001Assignee: Syntex (U.S.A.) LLCInventors: Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
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Patent number: 6316490Abstract: In accordance with the present invention, a novel class of substituted aryl compounds (containing ether, ester, amide, ketone or thioether substitution) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect, compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of displacing one or more acetylcholine receptor ligands, e.g., 3H-nicotine, from mammalian neuronal membrane binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors.Type: GrantFiled: July 8, 1997Date of Patent: November 13, 2001Assignee: Merck & Co., Inc.Inventors: Jean-Michel Vernier, Ian A. McDonald
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Patent number: 6316467Abstract: Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis.Type: GrantFiled: November 16, 1998Date of Patent: November 13, 2001Assignee: American Home Products CorporationInventor: Thomas J. Commons
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Publication number: 20010039290Abstract: Novel aromatic heterocyclic compounds inhibit cytokines production involved in immunoregulation and inflammation such as interleukin-1 and tumor necrosis factor production. The compounds are therefore useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.Type: ApplicationFiled: March 14, 2001Publication date: November 8, 2001Inventors: John R. Regan, Eugene R. Hickey, Neil Moss, Charles L. Cywin, Christopher Pargellis, Thomas A. Gilmore
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Patent number: 6303652Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.Type: GrantFiled: March 19, 1999Date of Patent: October 16, 2001Assignee: Hughes InstituteInventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
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Patent number: 6294575Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.Type: GrantFiled: October 16, 2000Date of Patent: September 25, 2001Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
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Patent number: 6281211Abstract: This invention is related to substituted semicarbazides represented by Formula (I) or a pharmaceutically acceptable salt or prodrug thereof, wherein: R1 and R2 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; R3, R4, R5 and R6 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl, or R3 and R4 is defined as above, and R5 and R6 together with the nitrogen atom to which they are attached form a heterocycle, including piperidine, piperazine, morpholine; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one of O, S, NR7, CH2, C(O), NR7C(O), C(O)NR7, SO, SO2 or a covalent bond; where R7 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; n isType: GrantFiled: September 21, 2000Date of Patent: August 28, 2001Assignee: Euro-Celtique S.A.Inventors: Sui Xiong Cai, Nancy C. Lan, Soo Hong-Bae
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Patent number: 6242432Abstract: Compounds or compositions containing compounds of the formula A-(X1—NO2)to or salts thereof, for the preparation of antithrombotic medications wherein “to” is the integer 1 or 2X1 is an alkylene connecting bridge and “A” is the residue of timolol or analapril.Type: GrantFiled: May 11, 1999Date of Patent: June 5, 2001Assignee: Nicox S.A.Inventor: Piero del Soldato
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Patent number: 6221865Abstract: Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2—, and (i) heterocyclic-L2—; R2 is selected from (a) (b) —C(O)NH—CH(R14)—C(O)OR15, (d) —C(O)NH—CH(R14)—C(O)NHSO2R16, (e) —C(O)NH—CH(R14)-tetrazolyl, (f) —C(O)NH-heterocyclic, and (g) —C(O)NH—CH(R14)—C(O)NR17R18; R3 is substituted or unsubstituted heterocyclic or aryl, substituted or unsubstituted cycloalkyl or cycloalkenyl, and —P(W)RR3RR3′; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) —L4—N(R5)—L5—, (b) —L4—O—L5—, (c) —L4—S(O)n—L5—(d) —L4—L6—C(W)—N(R5)&mdType: GrantFiled: May 7, 1998Date of Patent: April 24, 2001Assignee: University of PittsburghInventors: Said M. Sebti, Andrew D. Hamilton, Kenneth J. Barr, Stephen A. Fakhoury, Stephen J. O'Connor, Saul H. Rosenberg, Wang Shen, Bryan K. Sorensen, Gerard M. Sullivan, James T. Wasicak, Kenneth J. Henry, Le Wang
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Patent number: 6211176Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: July 1, 1999Date of Patent: April 3, 2001Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 6201016Abstract: Enantiomerically enriched disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.Type: GrantFiled: February 17, 1995Date of Patent: March 13, 2001Assignee: CytoMed IncorporatedInventors: Xiong Cai, Gurmit Grewal, Sajjat Hussoin, Aberra Fura, Ralph Scannell, Tesfaye Biftu
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Patent number: 6169094Abstract: A composition is provided comprising an antipsychotic effective amount of (S)(−)-amisulpride, (S)-(−)-4-amino-N-[(1-ethylpyrrolidin-2-yl)methyl]-5-ethylsulfonyl)-2-methoxybenzamide. A preferred composition comprises the (D)-tartrate salt of (S)(−)-amisulpride. The (S)(−) enantiomer exhibits antipsychotic properties and administration of the specific enantiomer reduces adverse side effects by reducing toxicity.Type: GrantFiled: July 14, 1998Date of Patent: January 2, 2001Assignee: Sanofi-SynthelaboInventors: Ghislaine Perrault, Hans Schoemaker, Jo{umlaut over (e)}l Miget
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Patent number: 6159973Abstract: The subject of the invention is the compounds of formula (I):Q(CH.sub.2).sub.a --(X.sub.1).sub.b --Q.sub.1 --Q.sub.2 --C(X.sub.2)--N(R.sub.1)(R.sub.2) (I)in which:Q represents an aryl radical,X.sub.1 represents oxy, thio, sulphinyl or sulphonyl,X.sub.2 represents oxygen or sulphur,Q.sub.1 represents a cyclopropanediyl radical,Q.sub.2 represents an arylene radical,R.sub.1 and R.sub.2 represent:either a hydrogen atom or a hydrocarbon radicalor one of the groupsR.sub.3 --C.dbd.X.sub.3, (R.sub.3).sub.2 --P.dbd.X.sub.3, T.sub.2 --R.sub.5 or S(O).sub.j --N(R.sub.6)(R.sub.7)in which X.sub.3 represents an oxygen atom or a sulphur atom, T.sub.2 represents a bivalent oxy, carbonyl or oxycarbonyl group and j is equal to 0, 1 or 2,their preparation process and their use as pesticides.Type: GrantFiled: July 21, 1999Date of Patent: December 12, 2000Assignee: Hoechst Schering Agrevo S.A.Inventors: Jacques Demassey, Michel Gohar, Christian Wehrey
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Patent number: 6160010Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.Type: GrantFiled: July 22, 1999Date of Patent: December 12, 2000Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
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Patent number: 6147224Abstract: Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.Type: GrantFiled: October 1, 1998Date of Patent: November 14, 2000Assignee: Allergan Sales, Inc.Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
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Patent number: 6124277Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.Type: GrantFiled: March 11, 1999Date of Patent: September 26, 2000Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 6072075Abstract: Trisubstituted N-protected guanidines and methods for use as guanidinylating reagents to yield N-protected guanidine derivatives.Type: GrantFiled: May 22, 1997Date of Patent: June 6, 2000Assignee: The Regents of the University of CaliforniaInventors: Murray Goodman, Konrad Feichtinger, Todd T. Romoff
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Patent number: 6017917Abstract: Guanidine derivatives of the formula: ##STR1## wherein R.sup.1 is [di(lower)alkylamino](lower)alkyl, morpholinyl(lower)alkyl, lower alkylpiperazinyl or [lower alkylpyrrolidinyl](lower)alkyl,R.sup.2 is halogen, lower alkyl or lower alkoxy, andR.sup.3 is halogen, lower alkyl, lower alkoxy or mono(or di or tri)halo(lower)alkyl,and pharmaceutically acceptable salts thereof which are useful as a medicament.Type: GrantFiled: June 26, 1998Date of Patent: January 25, 2000Assignee: Fujisawa Pharamceutical Co., Ltd.Inventors: Atsushi Kuno, Yoshikazu Inoue, Kumi Yamasaki
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Patent number: 5994507Abstract: A method for binding albumin by contacting an aqueous liquid containing an albumin with an albumin-binding compound is selected from albumin-binding compounds containing the scaffold --CO--NH--C(.dbd.C--)--CO--, and conjugates that are capable of binding albumin and exhibiting the scaffold --CO--NH--C(.dbd.C--)--CO--.Type: GrantFiled: December 31, 1997Date of Patent: November 30, 1999Assignee: Amersham Pharmacia Biotech ABInventors: .ANG.ke Pilotti, Tor Regberg, Christel Ellstrom, Charlotta Lindqvist, Ann Eckersten, Lars Fagerstam
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Patent number: 5939332Abstract: Novel analogs of phencyclidine (PCP) are disclosed. The analogs are capable of reacting with anti-PCT antibodies and are useful in immunoassays.The following analogs are described: ##STR1## wherein wherein X is --OH or a reporter molecule selected from the group consisting of aminofluorescein and aminomethylfluorescein and n is an integer between 1 and 10, inclusive.Type: GrantFiled: February 27, 1998Date of Patent: August 17, 1999Assignee: Roche Diagnostics Corp.Inventors: James C. Lee, Luis Fernando Del Corral, Richard A. Clark, Pedro A. Bonilla
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Patent number: 5922770Abstract: Novel peptide derivatives, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are disclosed. The peptides have the formula (I): ##STR1## wherein a, b, A, R.sup.1, L.sup.1, D, R.sup.3, R.sup.4, R.sup.2, L.sup.2, E and G are as defined in the specification. These peptides exhibit improved resistance to proteolytic degradation, and hence, improved bioavailability.Type: GrantFiled: July 17, 1997Date of Patent: July 13, 1999Assignee: Novo Nordisk A/SInventors: Bernd Peschke, Michael Ankersen, Thomas Kruse Hansen, Henning Th.o slashed.gersen
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Patent number: 5919934Abstract: Disclosed are bisaminothiol and amino compounds with appended pharmacophores, complexes of these compounds with .sup.99m Tc(V)0, Re(V)0, In.sup.+3, .sup.67 Ga.sup.+3, .sup.90 Y.sup.+3, .sup.109 Pd.sup.+2 or .sup.105 Rh.sup.+3, and pharmaceutical compositions containing the complexes. Also disclosed are methods of diagnosing a mammal for the presence of a mammalian tumor, methods for in vitro detection of a cancer cell in a mammalian tissue sample, and methods of treating a mammal having a tumor.Type: GrantFiled: February 19, 1997Date of Patent: July 6, 1999Assignee: The George Washington UniversityInventors: Christy Seith John, Benjamin Byung-Duk Lim
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Patent number: 5907039Abstract: Amino alcohol derivatives with a primary amino group or a substituted amino group influence the synthesis of glycolipids and have antiviral, antitumor, metastasis inhibiting and neural cell growth enhancing functions. The amino alcohol derivatives are useful in preparing 2-acylamino alcohol derivatives.Type: GrantFiled: December 9, 1996Date of Patent: May 25, 1999Assignee: Seikagaku Kogyo Kabushiki KaishaInventors: Masayuki Jinbo, Hidekazu Oyamada, Jinichi Inokuchi
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Patent number: 5885985Abstract: Guanidine derivatives of formula I ##STR1## wherein R.sup.8 represents hydrogen, halogen, alkyl C1 to 6, nitro, trifluoromethyl, thioalkyl C1 to 6, hydroxy, alkoxy C1 to 6, or a group selected from --NR.sup.4 R.sup.5, --O(CH.sub.2).sub.p Q, --(CH.sub.2).sub.m OQ, --(CH.sub.2).sub.m NR.sup.1 R.sup.2, --O(CH.sub.2).sub.m NR.sup.1 R.sup.2, --NHCO(CH.sub.2).sub.m NH(CH.sub.2).sub.n Q or --(CH.sub.2).sub.p CONR.sup.1 R.sup.2, or R.sup.8 represents the group A--CO--B; R.sup.9 represents hydrogen, halogen, alkyl C1 to 6, nitro or trifluoromethyl;and R.sup.1, R.sup.2, R.sup.4, R.sup.5, n, m, p, Q, A, B, and W are as defined in the specification, are described together with processes for their manufacture and compositions containing them. Compounds of formula I are useful in therapy.Type: GrantFiled: September 21, 1995Date of Patent: March 23, 1999Assignee: Astra AktiebolagInventors: James E. Macdonald, Robert Gentile, Robert J. Murray
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Patent number: 5863903Abstract: The present invention relates to hydroxy alkyl piperidine compounds and pharmaceutical compositions thereof which can be used to treat diabetes.Type: GrantFiled: March 14, 1995Date of Patent: January 26, 1999Assignee: Novo Nordisk A/SInventors: Karsten Lundgren, Ole Kirk
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Patent number: 5783576Abstract: New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.Type: GrantFiled: August 9, 1996Date of Patent: July 21, 1998Assignee: Boehringer Ingelheim KGInventors: Otto Roos, Georg Speck, Walter Losel, Dietrich Arndts, Wolf-Dietrich Bechtel
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Patent number: 5776972Abstract: Pharmaceutical preparations which are suitable for the treatment of inflammatory bowel disorders and contain at least one compound of the formula I ##STR1## in which R.sup.1 is Ar, cycloalkyl having 3-7 C atoms or cycloalkylalkyl having 4-8 C atoms,R.sup.2 is Ar, orR.sup.1 and R.sup.2 together are ##STR2## R.sup.3 is H, OH, OA or A, R.sup.4 is A or phenyl which can optionally be mono- or disubstituted by Hal, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A and/or NA.sub.2,R.sup.5 is OH, CH.sub.2 OH,R.sup.6 and R.sup.7 in each case independently of one another are H, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or methylenedioxy, with the oxy groups bonded to adjacent carbons on the ring,A is alkyl having 1-7 C atoms,Ar is a mono- or bicyclic aromatic radical which can optionally contain an N, O or S atom in the ring and can be mono-, di- or trisubstituted by A, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA and/or NHCONH.sub.2,D is CH.sub.Type: GrantFiled: June 27, 1996Date of Patent: July 7, 1998Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Andrew Barber, Christoph Seyfried, Gerd Bartoszyk, Rudolf Gottschlich
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Patent number: 5770624Abstract: Particularly the invention relates to the compounds of formula I ##STR1## wherein Ar represents carbocyclic aryl, heterocyclic aryl or biaryl;R.sub.1 represents lower alkyl, cycloalkyl, aryl-lower alkyl, lower alkoxy-lower alkyl, aryl, cycloalkyl-lower alkyl, halo-lower alkyl;R.sub.2 represents hydrogen or lower alkyl;R.sub.3 and R.sub.4 represent independently hydrogen, lower alkyl, lower alkoxy, halo, hydroxy, acyloxy, lower alkoxy-lower alkoxy, trifluoromethyl or cyano; or R.sub.3 and R.sub.4 together represent lower allylenedioxy;n represents an integer from 1 to 5;pharmaceutically acceptable prodrug derivatives; and pharmaceutically acceptable salts thereof; methods for preparation thereof;pharmaceutical compositions comprising said compounds; and a method of inhibiting TNF-alpha activity and matrix-degrading metalloproteinases in mammals using such compounds.Type: GrantFiled: December 10, 1996Date of Patent: June 23, 1998Assignee: Novartis Corp.Inventor: David Thomas Parker
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Patent number: 5756557Abstract: A method for preparing a polyurethane foam which comprises reacting an organic polyisocyanate and a polyol in the presence of a blowing agent, a cell stabilizer and a catalyst composition comprising a compound represented by the following formula I or II, or any blend of compounds I and II.Type: GrantFiled: May 6, 1997Date of Patent: May 26, 1998Assignee: Air Products and Chemicals, Inc.Inventors: Michael John Kimock, Mark Leo Listemann
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Patent number: 5731434Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.Type: GrantFiled: June 1, 1995Date of Patent: March 24, 1998Assignee: Abbott LaboratoriesInventors: Martin Winn, Steven A. Boyd, Charles W. Hutchins, Hwan-Soo Jae, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Bryan K. Sorensen
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Patent number: 5703093Abstract: Tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.Type: GrantFiled: May 31, 1995Date of Patent: December 30, 1997Assignee: Cytomed, Inc.Inventors: Xiong Cai, Aberra Fura, Changgeng Qian
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Patent number: 5703076Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 25, 1995Date of Patent: December 30, 1997Assignee: G. D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, Ko-Chung Lin, Gary A. DeCrescenzo, Donald J. Rogier, Jr., John N. Freskos
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Patent number: 5674864Abstract: Novel .alpha.-mercapto-alkylamines in all possible racemic, enantiomeric and diastereoisomeric forms of the formula ##STR1## wherein the substituents are as defined in the specification.Type: GrantFiled: May 24, 1995Date of Patent: October 7, 1997Assignee: Roussel UclafInventors: Fran.cedilla.ois Clemence, Odile Le Martret, Francis Petit
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Method for controlling emesis caused by chemotherapeutic agents and antiemetic agents useful therein
Patent number: 5646303Abstract: A method for alleviating emesis caused by chemotherapy which comprises administering an antiemetic agent or a pharmaceutically acceptable salt thereof to a patient in conjunction with the administration of a chemotherapeutic agent, said antiemetic agent being represented by the formula (I) ##STR1## wherein Z represents a substituent such as a lower alkyl group, a methoxyethoxymethyl group, or a benzoylmethyl group; or Z in conjunction with the adjacent position represents the atoms necessary to complete a 5 to 7 membered saturated or unsaturated oxygen-containing ring; R represents a hydrogen atom, a halogen atom, a lower alkyl group, a cycloalkyl group, a lower alkoxy group, an amino group, a lower alkyl-substituted amino group, an acylamido group, a sulfamoyl group, a sulfonamido group or a nitro group; n is an integer of 1 to 3; W is a straight chain or branched chain alkylene group of 1 to 4 carbon atoms; and X represents the atoms necessary to complete a 5 or 6 membered ring; said antiemetic agent beingType: GrantFiled: September 20, 1988Date of Patent: July 8, 1997Assignee: Pharmacia Inc.Inventors: Jung-Hui Sun, Chih-Yun Johnny Tu -
Patent number: 5607950Abstract: The invetion is a method of treating irritable bowel syndrome with a compound selected from the formula ##STR1## wherein R, R.sup.1, m, n p are as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 10, 1994Date of Patent: March 4, 1997Assignee: Pfizer Inc.Inventors: David Alker, Peter E. Cross, Alexander R. Mackenzie
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Patent number: 5605926Abstract: The present invention relates to new trifluoromethyl-containing pseudopeptides of the general formula (I) ##STR1## in which W, A, B, D, E, R.sub.1, R.sub.2 and R.sub.3 have the meaning as outlined of their making and use as pharmaceuticals.Type: GrantFiled: April 10, 1995Date of Patent: February 25, 1997Assignee: Bayer AktiengesellschaftInventors: Dieter H abich, Wolfgang R oben, Jutta Hansen, Arnold Paessens
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Patent number: 5599994Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.The method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.Type: GrantFiled: June 7, 1995Date of Patent: February 4, 1997Assignee: Pharm-Eco Laboratories, Inc.Inventors: Biman Pal, Siya Ram, Yesh P. Sachdeva, Jaechul Shim, Salah A. Zahr, Emile Al-Farhan, Richard L. Gabriel
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Patent number: 5591856Abstract: Novel (pyrrolidinyl)phenyl carbamates and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the carbamates and related compounds, or compositions thereof are disclosed.Type: GrantFiled: January 10, 1995Date of Patent: January 7, 1997Assignee: Hoechst Roussel Pharmaceuticals Inc.Inventors: David G. Wettlaufer, Peter A. Nemoto
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Patent number: 5571832Abstract: Compounds comprising a pyrrolidinyl ring are disclosed for use in the treatment of cerebral ischemia.Type: GrantFiled: June 20, 1994Date of Patent: November 5, 1996Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Brian R. de Costa, Wayne D. Bowen, Xiao-Shu He, Lilian Radesca, Kenner C. Rice
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Patent number: 5565494Abstract: This invention provides certain benzenesulfonamide derivatives and methods for using them in the treatment of susceptible neoplasms in mammals. Also provided are certain novel pharmaceutical formulations employing these benzenesulfonamide derivatives in combination with a carrier, and processes for preparing the benzenesulfonamide derivatives.Type: GrantFiled: March 10, 1995Date of Patent: October 15, 1996Assignee: Eli Lilly and CompanyInventors: Gerald B. Grindey, Cora S. Grossman, J. Jeffry Howbert, Karen L. Lobb, James E. Ray, John E. Toth
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Patent number: 5563168Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.Type: GrantFiled: June 16, 1995Date of Patent: October 8, 1996Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 5559130Abstract: A compound selected from the group consisting of all possible racemic, enantiomeric and diastereoisomeric forms of a compound of the formula ##STR1## wherein E and G together form a group selected from the group: ##STR2## consisting of a) ##STR3## or, if appropriate, its tautomer ##STR4## and ##STR5## or E is --COOR.sub.3 and G is ##STR6## wherein A, Y, R, Ra, R.sub.1 and R.sub.2 are as defined in the specification.Type: GrantFiled: November 29, 1994Date of Patent: September 24, 1996Assignee: Roussel UclafInventors: Fran.cedilla.ois Clemence, Michel Fortin, Odile Le Martret
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Patent number: 5525617Abstract: Fibrinogen receptor antagonists having the formula ##STR1## for example ##STR2##Type: GrantFiled: August 24, 1994Date of Patent: June 11, 1996Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Melissa S. Egbertson, Laura Birchenough, Laura Vassallo
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Patent number: 5523325Abstract: This invention relates to amidrazones, insecticidal amidrazone compositions, and methods of using such compositions.Type: GrantFiled: September 9, 1993Date of Patent: June 4, 1996Inventor: Richard M. Jacobson